Assay Detail
Binding
CHEMBL681945
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Non-competitive displacement of [35S]TBPS from picrotoxin binding site found in heterogeneous Gamma-aminobutyric acid A receptor in rat brain membranes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Neurosteroid analogues. 9. Conformationally constrained pregnanes: structure-activity studies of 13,24-cyclo-18,21-dinorcholane analogues of the GABA modulatory and anesthetic steroids (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.26 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL210952 | ELTANOLONE | 2.0 | 1 | 7.15 |
| CHEMBL3137969 | — | — | 1 | 6.98 |
| CHEMBL3137966 | — | — | 1 | 6.71 |
| CHEMBL3137971 | — | — | 1 | 6.61 |
| CHEMBL3137962 | — | — | 1 | 6.57 |
| CHEMBL3137960 | — | — | 1 | 6.52 |
| CHEMBL3137961 | — | — | 1 | 6.48 |
| CHEMBL3137959 | — | — | 1 | 6.48 |
| CHEMBL3138304 | — | — | 1 | 6.43 |
| CHEMBL3138306 | — | — | 1 | 6.29 |
| CHEMBL3138273 | — | — | 1 | 6.05 |
| CHEMBL3137970 | — | — | 1 | 5.90 |
| CHEMBL3138399 | — | — | 1 | 5.84 |
| CHEMBL3137958 | — | — | 1 | 5.80 |
| CHEMBL3138305 | — | — | 1 | 5.75 |
| CHEMBL3138309 | — | — | 1 | 5.49 |
| CHEMBL3138269 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL210952 | ELTANOLONE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3137969 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL3137966 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL3137971 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL3137962 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL3137960 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL3137961 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL3137959 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL3138304 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL3138306 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL3138273 | — | IC50 | = | 899.0 | nM | 6.05 |
| CHEMBL3137970 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL3138399 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL3137958 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL3138305 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL3138309 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL3138269 | — | IC50 | = | 4750.0 | nM | 5.32 |